Selective liver X receptor modulators (SLiMs): What use in human health?

被引：101

作者：

Viennois, Emilie ^{[1
,2
,3
]}

Mouzat, Kevin ^{[4
]}

Dufour, Julie ^{[1
,2
,3
]}

Morel, Laurent ^{[1
,2
,3
]}

Lobaccaro, Jean-Marc ^{[1
,2
,3
]}

Baron, Silvere ^{[1
,2
,3
]}

机构：

[1] Clermont Univ, Univ Blaise Pascal, F-63000 Clermont Ferrand, France

[2] CNRS, UMR 6247, GReD, F-63177 Clermont Ferrand, France

[3] Ctr Rech Nutr Humaine Auvergne, F-63000 Clermont Ferrand, France

[4] Hop Univ Caremeau, Biochim Lab, F-30029 Nimes, France

来源：

MOLECULAR AND CELLULAR ENDOCRINOLOGY | 2012年 / 351卷 / 02期

关键词：

Liver X receptors; Pharmacology; SLiMs; Human pathologies; Cholesterol; Nuclear receptors; REVERSE CHOLESTEROL TRANSPORT; ELEMENT-BINDING PROTEIN; LXR-ALPHA; NUCLEAR RECEPTOR; PROSTATE-CANCER; OXYSTEROL RECEPTOR; HUMAN KERATINOCYTES; NATURAL-PRODUCT; BREAST-CANCER; AGONIST TREATMENT;

D O I：

10.1016/j.mce.2011.08.036

中图分类号：

Q2 [细胞生物学];

学科分类号：

071013 [干细胞生物学];

摘要：

Liver X receptors (LXR) are members of the nuclear receptor family. As activated transcription factors, their putative association with human diseases makes them promising pharmacological targets because of the large potential to develop ligands. LXR are mainly considered as intracellular cholesterol "sensors" whose activation leads to decreased plasma cholesterol. They also modulate numerous physiological functions: fatty acid synthesis and metabolism, glucose homeostasis, steroidogenesis, immunity, and neurological homeostasis. LXR-deficiency in mouse results in several phenotypes mimicking pathological conditions in humans. This review will be focused on the various natural and synthetic LXR agonists and antagonists. Putative clinical targets including atherosclerosis, diabetes. Alzheimer's disease, skin disorders, and cancer will be covered. (C) 2011 Elsevier Ireland Ltd. All rights reserved.

引用

页码：129 / 141

页数：13

共 127 条

[1]

Genetic variability at the LXR gene (NR1H2) may contribute to the risk of Alzheimer's disease [J].

Adighibe, Omanma ;

Arepalli, Sampath ;

Duckworth, Jaime ;

Hardy, John ;

Wavrant-De Vrieze, Fabienne .

NEUROBIOLOGY OF AGING, 2006, 27 (10) :1431-1434

[2]

Lipid-activated transcription factors control bile acid glucuronidation [J].

Barbier, Olivier ;

Trottier, Jocelyn ;

Kaeding, Jenny ;

Caron, Patrick ;

Verreault, Melanie .

MOLECULAR AND CELLULAR BIOCHEMISTRY, 2009, 326 (1-2) :3-8

[3]

Identification of 5α,6α-Epoxycholesterol as a Novel Modulator of Liver X Receptor Activity [J].

Berrodin, Thomas J. ;

Shen, Qi ;

Quinet, Elaine M. ;

Yudt, Matthew R. ;

Freedman, Leonard P. ;

Nagpal, Sunil .

MOLECULAR PHARMACOLOGY, 2010, 78 (06) :1046-1058

[4]

Novel role for the liver X nuclear receptor in the suppression of lung inflammatory responses [J].

Birrell, Mark A. ;

Catley, Matthew C. ;

Hardaker, Elizabeth ;

Wong, Sissie ;

Willson, Timothy M. ;

McCluskie, Kerryn ;

Leonard, Thomas ;

Farrow, Stuart N. ;

Collins, Jon L. ;

Haj-Yahia, Saleem ;

Belvisi, Maria G. .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2007, 282 (44) :31882-31890

[5]

A natural product ligand of the oxysterol receptor, liver X receptor [J].

Bramlett, KS ;

Houck, KA ;

Borchert, KM ;

Dowless, MS ;

Kulanthaivel, P ;

Zhang, YY ;

Beyer, TP ;

Schmidt, R ;

Thomas, JS ;

Michael, LF ;

Barr, R ;

Montrose, C ;

Eacho, PI ;

Cao, GQ ;

Burris, TP .

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2003, 307 (01) :291-296

[6]

Self-reported history of hypercholesterolaemia and gallstones and the risk of prostate cancer [J].

Bravi, F ;

Scotti, L ;

Bosetti, C ;

Talamini, R ;

Negri, E ;

Montella, M ;

Franceschi, S ;

La Vecchia, C .

ANNALS OF ONCOLOGY, 2006, 17 (06) :1014-1017

[7]

Antidiabetic action of a liver X receptor agonist mediated by inhibition of hepatic gluconeogenesis [J].

Cao, GQ ;

Liang, Y ;

Broderick, CL ;

Oldham, BA ;

Beyer, TP ;

Schmidt, RJ ;

Zhang, YY ;

Stayrook, KR ;

Suen, C ;

Otto, KA ;

Miller, AR ;

Dai, JN ;

Foxworthy, P ;

Gao, H ;

Ryan, TP ;

Jiang, XC ;

Burris, TP ;

Eacho, PI ;

Etgen, GJ .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2003, 278 (02) :1131-1136

[8]

The liver X receptor (LXR) and hepatic lipogenesis - The carbohydrate-response element-binding protein is a target gene of LXR [J].

Cha, Ji-Young ;

Repa, Joyce J. .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2007, 282 (01) :743-751

[9]

Liver X Receptor Is a Therapeutic Target for Photoaging and Chronological Skin Aging [J].

Chang, Ken C. N. ;

Shen, Qi ;

Oh, Inn Gyung ;

Jelinsky, Scott A. ;

Jenkins, Susan F. ;

Wang, Wei ;

Wang, Yihe ;

LaCava, Margaret ;

Yudt, Matthew R. ;

Thompson, Catherine C. ;

Freedman, Leonard P. ;

Chung, Jin Ho ;

Nagpal, Sunil .

MOLECULAR ENDOCRINOLOGY, 2008, 22 (11) :2407-2419

[10]

Enzymatic reduction of oxysterols impairs LXR signaling in cultured cells and the livers of mice [J].

Chen, Wenling ;

Chen, Guoxen ;

Head, Daphne L. ;

Mangelsdorf, David J. ;

Russell, David W. .

CELL METABOLISM, 2007, 5 (01) :73-79

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